Preparation of Therapeutic Dose of 177Lu-DOTA-TATE Using a Novel Single Vial Freeze-dried Kit: A Comparison with ‘In-situ’ Preparation at Hospital Radiopharmacy
Tapas Das, Sharmila Banerjee, Ajit Shinto, K.K. Kamaleshwaran and H.D. Sarma
Affiliation: Isotope Applications and Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai 400 085, India.
Keywords: 177Lu-DOTA-TATE, Freeze-dried DOTA-TATE kit, Neuroendocrine cancers, PRRT.
Objective: Patient dose of 177Lu-DOTA-TATE, used for providing radiotherapeutic treatment to the patients suffering
from cancers of neuroendocrine origin, could be prepared at the hospital radiopharmacy either ‘in-situ’ or by using freezedried
kits. The objective of the present work is to formulate and evaluate a single vial freeze-dried DOTA-TATE kit,
which is capable of producing up to 7.4 GBq (200 mCi) dose of 177Lu-DOTA-TATE and to compare the two methodologies
presently used for the preparation of the agent.
Experimental: Freeze-dried DOTA-TATE kits, comprising a lyophilized mixture of DOTA-TATE, gentisic acid and
ammonium acetate, were prepared and used for the formulation of patient doses of 177Lu-DOTA-TATE. The kits were
subjected to detailed radiochemical evaluation and the shelf-life of the kits was determined. The pharmacokinetic behavior
of the agent was studied in normal Wistar rats. These kits were utilized for treating the patients suffering from various
types of neuroendocrine cancers.
Results: The freeze-dried kits were used for the preparation of up to 7.4 GBq (200 mCi) therapeutic doses of 177Lu-
DOTA-TATE with a radiochemical purity of >99% and were found to have sufficiently long shelf-life. Biological studies
carried out in normal Wistar rats exhibited no significant accumulation of activity in any of the vital organs/tissue except
in kidneys and non-accumulated activity showed major renal clearance. Clinical studies carried out in cancer patients exhibited
accumulation of activity in the cancerous lesions and metastatic sites.
Conclusion: The kit was useful for the convenient preparation of therapeutic dose of 177Lu-DOTA-TATE, suitable for human
administration. The use of kit is expected to reduce the batch failure and radiation exposure to the working personnel.
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